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AZD-1656

AZD-1656

产品编号 T26712   CAS 919783-22-5
别名: AZD 1656

AZD-1656 是口服有效的葡萄糖激酶选择性激活剂,EC50为 60 nM。AZD1656在2 型糖尿病中有研究的价值。

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AZD-1656 Chemical Structure
AZD-1656, CAS 919783-22-5
规格 价格/CNY 货期 数量
1 mg ¥ 752 现货
5 mg ¥ 1,860 现货
10 mg ¥ 2,980 现货
25 mg ¥ 5,930 现货
50 mg ¥ 7,880 5日内发货
1 mL * 10 mM (in DMSO) ¥ 1,960 现货
产品目录号及名称: AZD-1656 (T26712)
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选择批次  
纯度: 99.37%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 AZD-1656 is a glucokinase activator (GKA) that can cause dose-limiting hypoglycemia in normal animals used in embryofetal development studies and type 2 diabetes.
靶点活性 glucokinase:60 nM (EC50)
体内活性 The gkdel/wt mouse was used as an alternative rodent strain for embryofetal development studies with AZD-1656. Heterozygous global knockout gkdel/wt females were dosed with 20, 50, or 130 mg/kg/day of AZD-1656 or vehicle for a minimum of 14 consecutive days before mating with wild-type males and throughout organogenesis. Maternal effects were confined to slightly reduced food consumption, reduced body weight gain, and the pharmacologic effect of decreased plasma glucose. Fetuses were genotyped. Fetal weights at the high dose were slightly reduced but there was no effect on fetal survival. There were two specificmajormalformations, omphalocele and right-sided aortic arch, with increased fetal incidence in mid- and high-dose fetuses (e.g., omphalocele fetal incidence of 0.6, 0.7, 4.6, and 2% across the dose groups) plus increased incidences of minor abnormalities and variants indicative of either delayed or disturbed development. Fetal weight and abnormalities were unaffected by fetal genotype. The fetal effects are considered hypoglycemia related. There was no effect on embryofetal survival in the gkdel/wt mouse at AZD-1656 exposures[1].
别名 AZD 1656
分子量 478.5
分子式 C24H26N6O5
CAS No. 919783-22-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 250 mg/mL (522.47 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0899 mL 10.4493 mL 20.8986 mL 52.2466 mL
5 mM 0.418 mL 2.0899 mL 4.1797 mL 10.4493 mL
10 mM 0.209 mL 1.0449 mL 2.0899 mL 5.2247 mL
20 mM 0.1045 mL 0.5225 mL 1.0449 mL 2.6123 mL
50 mM 0.0418 mL 0.209 mL 0.418 mL 1.0449 mL
100 mM 0.0209 mL 0.1045 mL 0.209 mL 0.5225 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Krentz AJ, et al. Effect of exogenously administered glucagon versus spontaneous endogenous counter-regulation on glycaemic recovery from insulin-induced hypoglycaemia in patients with type 2 diabetes treated with a novel glucokinase activator, AZD1656, and metformin. Diabetes Obes Metab. 2014 Nov;16(11):1096-101. 2. Terri Mitchard, et al. The novel use of a heterozygous knockout mouse for embryofetal development assessment of a glucokinase activator. Birth Defects Res B Dev Reprod Toxicol. 2014 Apr;101(2):152-61. 3. Brian E Ford, et al. Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge. Diabetes Obes Metab. 2020 Jun 10. 4. Medicinal Chemistry, et al. Design and Development of the Glucokinase Activator AZD1656. Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 1, 185-220.
PF-04991532 Cefetrizole ML266 PF-04937319 WAY-640509 PFK-015 AMG-1694 WAY-297848

相关化合物库

该产品包含在如下化合物库中:
口服活性化合物库 药物功能重定位化合物库 代谢化合物库 已知活性化合物库 临床期小分子药物库 经典已知活性库 抗癌细胞代谢库 糖酵解化合物库 抗病毒库 ReFRAME 相关化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AZD-1656 919783-22-5 Metabolism Glucokinase Hexokinase IV AZD1656 G6pc G6P ChREBP-β hypoglycemia AZD 1656 inhibit Inhibitor Hexokinase D epinephrine glucagon antihyperglycemic inhibitor

 

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